Formulation and evaluation of thermoreversible mucoadhesive nasal gels of metoclopramide hydrochloride

The prolonged residence of drug formulation in the nasal cavity is of utmost importance for intranasal drug delivery. The objective of the present investigation was to develop a mucoadhesive in situ gel with reduced nasal mucocilliary clearance in order to improve the bioavailability of the antiemetic drug, metoclopramide hydrochloride. The in situ gelation upon contact with nasal mucosa was conferred via the use of the thermogelling Pluronic flake 127 (18%). Mucoadhesion was modulated via the use of hydroxy propyl methyl cellulose (HPMC), sodium carboxy methyl cellulose (Na CMC) and sodium alginate (Na-alginate) whereas drug release was modified by varying concentrations of polyethylene glycol 6000 (PEG 6000). The results revealed that the different mucoadhesives increased the gel viscosity but reduced its sol gel transition temperatures. The increase in viscosity was highest in formulations with Na-alginate and lowest in formulations with HPMC. PEG 6000 significantly decreased mucoadhesive strength of formula containing 0.3% HPMC (776.6 ± 19.55 to 713.6 ± 5.03), 0.2% Na CMC (656 ± 11.13 to 575 ± 9.07) and 0.2% Na-alginate (659 ± 11.13 to 618.3 ± 9.45) whereas the gelation temperature increased by 3 to 4 °C. 100% of drug diffusion was found at four hours for formulation F5, F9, and F12. Formulation F5 showed maximum permeability (0.00949 ± 0.00021 mg.cm/min) than other formulation containing PEG6000. This study concluded the potential use of mucoadhesive in situ nasal gel in terms of ease of administration, accuracy of dosing, prolonged nasal residence and improved nasal bioavailability.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Formulation and evaluation of thermoreversible mucoadhesive nasal gels of metoclopramide hydrochloride

The prolonged residence of drug formulation in the nasal cavity is of utmost importance for intranasal drug delivery. The objective of the present investigation was to develop a mucoadhesive in situ gel with reduced nasal mucocilliary clearance in order to improve the bioavailability of the antiemetic drug, metoclopramide hydrochloride. The in situ gelation upon contact with nasal mucosa was conferred via the use of the thermogelling Pluronic flake 127 (18%). Mucoadhesion was modulated via the use of hydroxy propyl methyl cellulose (HPMC), sodium carboxy methyl cellulose (Na CMC) and sodium alginate (Na-alginate) whereas drug release was modified by varying concentrations of polyethylene glycol 6000 (PEG 6000). The results revealed that the different mucoadhesives increased the gel viscosity but reduced its sol gel transition temperatures. The increase in viscosity was highest in formulations with Na-alginate and lowest in formulations with HPMC. PEG 6000 significantly decreased mucoadhesive strength of formula containing 0.3% HPMC (776.6 ± 19.55 to 713.6 ± 5.03), 0.2% Na CMC (656 ± 11.13 to 575 ± 9.07) and 0.2% Na-alginate (659 ± 11.13 to 618.3 ± 9.45) whereas the gelation temperature increased by 3 to 4 °C. 100% of drug diffusion was found at four hours for formulation F5, F9, and F12. Formulation F5 showed maximum permeability (0.00949 ± 0.00021 mg.cm/min) than other formulation containing PEG6000. This study concluded the potential use of mucoadhesive in situ nasal gel in terms of ease of administration, accuracy of dosing, prolonged nasal residence and improved nasal bioavailability.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Formulation and evaluation of thermoreversible mucoadhesive nasal gels of metoclopramide hydrochloride

The prolonged residence of drug formulation in the nasal cavity is of utmost importance for intranasal drug delivery. The objective of the present investigation was to develop a mucoadhesive in situ gel with reduced nasal mucocilliary clearance in order to improve the bioavailability of the antiemetic drug, metoclopramide hydrochloride. The in situ gelation upon contact with nasal mucosa was conferred via the use of the thermogelling Pluronic flake 127 (18%). Mucoadhesion was modulated via the use of hydroxy propyl methyl cellulose (HPMC), sodium carboxy methyl cellulose (Na CMC) and sodium alginate (Na-alginate) whereas drug release was modified by varying concentrations of polyethylene glycol 6000 (PEG 6000). The results revealed that the different mucoadhesives increased the gel viscosity but reduced its sol gel transition temperatures. The increase in viscosity was highest in formulations with Na-alginate and lowest in formulations with HPMC. PEG 6000 significantly decreased mucoadhesive strength of formula containing 0.3% HPMC (776.6 ± 19.55 to 713.6 ± 5.03), 0.2% Na CMC (656 ± 11.13 to 575 ± 9.07) and 0.2% Na-alginate (659 ± 11.13 to 618.3 ± 9.45) whereas the gelation temperature increased by 3 to 4 °C. 100% of drug diffusion was found at four hours for formulation F5, F9, and F12. Formulation F5 showed maximum permeability (0.00949 ± 0.00021 mg.cm/min) than other formulation containing PEG6000. This study concluded the potential use of mucoadhesive in situ nasal gel in terms of ease of administration, accuracy of dosing, prolonged nasal residence and improved nasal bioavailability.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Sodium alginate microspheres containing multicomponent inclusion complex of domperidone

Sodium alginate microspheres of domperidone for intranasal systemic delivery were developed to eliminate first pass metabolism, improve patient compliance and obtain improved therapeutic efficacy in treatment of migraine, gastro-esophageal reflux and chemotherapy induced nausea and vomiting. Domperidone was encapsulated as ternary inclusion complex with β-cyclodextrin and citric acid to improve solubility. The phase solubility studies were performed in order to select suitable acid and ternary inclusion complex was prepared by kneading method. The complex was characterized by differential scanning calorimetry, X-ray diffraction and Fourier transform infrared spectroscopy. In vitro dissolution study was carried out in simulated nasal electrolyte solution, pH 6.4. The microspheres of optimised ternary inclusion complex were prepared by emulsification-cross-linking method and were evaluated for particle size, encapsulation efficiency, equilibrium swelling degree, in vitro mucoadhesion and in vitro drug release. The effect of various formulation variables such as drug loading, polymer concentration, crosslinking agent concentration and cross-linking time on microsphere characteristics were studied. The microspheres size range was 57.63-65.3 µm, whereas the percentage drug encapsulation was within the range 15-50 %. All microspheres showed good bioadhesive properties. The formulation variables influenced the drug release profile. The treatment of in vitro release kinetics with kinetic equations indicated that the domperidone release followed Higuchi's matrix model.Colegio de Farmacéuticos de la Provincia de Buenos Aire

In vitro absorption studies of acyclovir using natural permeation enhancers

Gastroretentive Delivery Systems are employed to improve the bioavailability of drugs which are absorbed through upper part of GIT, by increasing their retention time. Incorporation of permeability enhancers in the formulations of such drugs can further increase their bioavailability; however their use in the formulations is questionable due to the toxicity exhibited by them. Acyclovir is a class III drug having low oral bioavailability due to improper absorption. Mucoadhesive tablets of acyclovir containing natural permeation enhancers were prepared by direct compression and evaluated for mucoadhesion strength, in-vitro dissolution parameters and in-vitro absorption studies. The formulations containing Aloe vera extract showed increase in the mucoadhesion strength and retarded the drug release. The in-vitro absorption studies revealed that the formulations containing Aloe vera extract (Enhancement Ratio 1.94) and chausath prahar pippal (Enhancement Ratio 1.87) showed significant increase in the permeation of the drug. The studies led to the conclusion that by formulating mucoadhesive tablets of acyclovir containing natural permeation enhancers increased the permeability, thus proving to be the cheaper and easily available alternative to the other permeation enhancers.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Industrial Marketing

379.;xxviii.;24 c

Oral health status of Tibetan and local school children of Kushalnagar, Mysore district, India: A comparative study

The presence of migrants culturally different from inhabitants of the host country is now a widespread phenomenon. It is known that dietary habits and oral hygiene practices vary from country to country, which in turn has a profound effect on oral health. Objectives: To assess and compare the oral health status of Tibetan school children and local school children of Kushalnagar (Bylakuppe). Study design: A survey was conducted at Kushalnagar (Bylakuppe), in Mysore district, India to assess the oral health status of Tibetan school children (n = 300) and local school children (n = 300) and compared using World Health Organization oral health proforma (1997). Results: The proportional values are compared using chi-square test and the mean values are compared using Student′s t-test. Statistically significant results were obtained for soft tissue lesions, dental caries, malocclusion, and treatment needs. However, results were not significant when gingivitis was compared in the two populations. Conclusions: Tibetan school children showed higher prevalence of Angular cheilitis, gingival bleeding, dental caries experience, malocclusion, and treatment needs in comparison with non-Tibetans. Among the Tibetan school children, the requirement for two or more surface filling was more